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Assay Detail

CHEMBL4026640

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Agonist activity at human recombinant phosphorylated AMPK complex 8 alpha2/beta1/gamma2 expressed in baculovirus infected Sf21 cells assessed as phosphorylation of 5-FAM-labeled SAMS substrate preincubated for 30 mins in presence of AMPK activator followed by substrate addition measured after 60 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase.
Lan P, Romero FA, Wodka D, Kassick AJ, Dang Q, Gibson T, Cashion D, Zhou G, Chen Y, Zhang X, Zhang A, Li Y, Trujillo ME, Shao Q, Wu M, Xu S, He H, MacKenna D, Staunton J, Chapman KT, Weber A, Sebhat IK, Makara GM.
J Med Chem (2017) 60 : 9040 -9052
PubMed 29035567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.66 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4082745 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4082745 EC50 = 22.0 nM 7.66